Pharmacokinetics of morphine in cancer patients following oral administration of aqueous and controlled-release morphine at steady state.

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Controlled-release morphine sulfate tablet (MS-Contin: MS-C) has been reported to have the same analgesic effect on a twice-a-day regimen as aqueous morphine every 4hr.<BR>In this study, the pharmacokinetics of morphine and morphine-6-glucuronide (M-6-G) in cancer patients at steady state following oral administrations of three MS-C 10mg tablets every 12hr were compared with those following oral administrations of aqueous morphine (10mg) every 4hr.<BR>Elimination half-lives of morphine and M-6-G after administration of MS-C were found to be 2.58±0.85hr and 4.66±1.11hr, respectively, which were comparable to those after administration of aqueous morphine. On the other hand, absorption rate of morphine from MS-C was one-fourth of that obtained from the aqueous solution and the peak concentration from MS-C was less than three times that from the aqueous morphine and was observed about 3hr later compared with that from aqueous morphine solution. These results show that MS-C has sustained-release characteristics . The simulated curves of morphine and M-6-G plasma concentrations after MS-C administration were shown to be comparable to those after aqueous morphine administration. Moreover, in the two patients who received MS-C and aqueous morphine, the observed plasma concentration profiles were the same as the simulation.
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